Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 59, Issue 15, Pages 6015-6020Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201914826
Keywords
cancer; chromophores; fluorescent probes; imaging; vitamins
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Funding
- JSPS KAKENHI [JP18H04609, JP16H05099, JP26110005]
- SENTAN, JST
- Hoansha Foundation
- Daiichi Sankyo Foundation of Life Science
- JSPS Core-toCore program, A. Advanced Research Networks
- Ministry of Education, Culture, Sports, Science, and Technology, Japan [8007, JP19H05414]
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Folate receptors (FRs) are membrane proteins involved in folic acid uptake, and the alpha isoform (FR-alpha) is overexpressed in ovarian and endometrial cancer cells. For fluorescence imaging of FRs in vivo, the near-infrared (NIR) region (650-900 nm), in which tissue penetration is high and autofluorescence is low, is optimal, but existing NIR fluorescent probes targeting FR-alpha show high non-specific tissue adsorption, and require prolonged washout to visualize tumors. We have designed and synthesized a new NIR fluorescent probe, FolateSiR-1, utilizing a Si-rhodamine fluorophore having a carboxy group at the benzene moiety, coupled to a folate ligand moiety through a negatively charged tripeptide linker. This probe exhibits very low background fluorescence and afforded a tumor-to-background ratio (TBR) of up to 83 in FR-expressing tumor-bearing mice within 30 min. Thus, FolateSiR-1 has the potential to contribute to the research in the field of biology and the clinical medicine.
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